Phosphinic peptides, the first potent inhibitors of astacin, behave as extremely slow-binding inhibitors.

No abstract is available for this paper.

• Publication year

  1998

• Venue

  Biochemical Journal

• Publication date

  1998-04-15

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1042/BJ3310375PMID 9531473PMCID PMC1219364
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Bone Morphogenetic Protein-1: The Type I Procollagen C-Proteinase

  1996cited by this paper
• Development of the First Potent and Selective Inhibitor of the Zinc Endopeptidase Neurolysin Using a Systematic Approach Based on Combinatorial Chemistry of Phosphinic Peptides*

  1996cited by this paper
• Just add water! The effect of water on the specificity of protein-ligand binding sites and its potential application to drug design.

  1996cited by this paper
• Failure of ventral body wall closure in mouse embryos lacking a procollagen C-proteinase encoded by Bmp1, a mammalian gene related to Drosophila tolloid.

  1996cited by this paper
• Protection of the Hydroxyphosphinyl Function of Phosphinic Dipeptides by Adamantyl. Application to the Solid-Phase Synthesis of Phosphinic Peptides.

  1996cited by this paper
• Structure of astacin with a transition-state analogue inhibitor

  1996cited by this paper
• The C-proteinase that processes procollagens to fibrillar collagens is identical to the protein previously identified as bone morphogenic protein-1.

  1996cited by this paper
• The astacin family of metalloendopeptidases.

  1995cited by this paper
• Theoretical and practical aspects of proteinase inhibition kinetics.

  1995cited by this paper
• Crystal structure of a complex between Serratia marcescens metallo-protease and an inhibitor from Erwinia chrysanthemi.

  1995cited by this paper
• Development of Highly Potent and Selective Phosphinic Peptide Inhibitors of Zinc Endopeptidase 24-15 Using Combinatorial Chemistry (*)

  1995cited by this paper
• What makes a binding site a binding site?

  1995cited by this paper
• The metzincins — Topological and sequential relations between the astacins, adamalysins, serralysins, and matrixins (collagenases) define a super family of zinc‐peptidases

  1995cited by this paper
• Embryonic expression of mouse bone morphogenetic protein-1 (BMP-1), which is related to the Drosophila dorsoventral gene tolloid and encodes a putative astacin metalloendopeptidase.

  1994cited by this paper
• Refined 1.8 A X-ray crystal structure of astacin, a zinc-endopeptidase from the crayfish Astacus astacus L. Structure determination, refinement, molecular structure and comparison with thermolysin.

  1994cited by this paper
• Phosphinic peptide analogues as potent inhibitors of Corynebacterium rathayii bacterial collagenase.

  1994cited by this paper
• Three‐dimensional structure of the alkaline protease of Pseudomonas aeruginosa: a two‐domain protein with a calcium binding parallel beta roll motif.

  1993cited by this paper
• Cloning and expression of cDNA encoding Xenopus laevis bone morphogenetic protein-1 during early embryonic development.

  1993cited by this paper
• Implications of the three-dimensional structure of astacin for the structure and function of the astacin family of zinc-endopeptidases.

  1993cited by this paper
• Astacins, serralysins, snake venom and matrix metalloproteinases exhibit identical zinc‐binding environments (HEXXHXXGXXH and Met‐turn) and topologies and should be grouped into a common family, the ‘metzincins’

  1993cited by this paper
• Structure of astacin and implications for activation of astacins and zinc-ligation of collagenases

  1992cited by this paper
• Comprehensive medicinal chemistry

  1991cited by this paper
• The astacin family of metalloendopeptidases

  1991cited by this paper
• Fluorescent oligopeptide substrates for kinetic characterization of the specificity of Astacus protease.

  1990cited by this paper
• Thiol containing compounds and amino acid hydroxamates as reversible synthetic inhibitors of Astacus protease.

  1990cited by this paper
• Structure of chymotrypsin-trifluoromethyl ketone inhibitor complexes: comparison of slowly and rapidly equilibrating inhibitors.

  1990cited by this paper
• Binding energetics of phosphorus-containing inhibitors of thermolysin.

  1989cited by this paper
• Novel regulators of bone formation: molecular clones and activities.

  1988cited by this paper
• Possible role for water dissociation in the slow binding of phosphorus-containing transition-state-analogue inhibitors of thermolysin.

  1987cited by this paper
• The slow, tight binding of bestatin and amastatin to aminopeptidases.

  1985cited by this paper
• In vivo significance of kinetic constants of protein proteinase inhibitors.

  1984cited by this paper
• Inhibition of isocitrate lyase by 3-nitropropionate, a reaction-intermediate analogue.

  1982cited by this paper
• Tight-binding inhibitors-I. Kinetic behavior.

  1975cited by this paper

• Blocking Fas signaling in adipose tissue ameliorates obesity-associated inflammation, insulin resistance, and hepatosteatosis

  2024cites this paper
• Structural insights into latency of the metallopeptidase ulilysin (lysargiNase) and its unexpected inhibition by a sulfonyl-fluoride inhibitor of serine peptidases.

  2023cites this paper
• Phosphinic Peptides as Tool Compounds for the Study of Pharmacologically Relevant Zn-Metalloproteases.

  2022cites this paper
• A novel assay based on pre-equilibrium titration curves for the determination of enzyme inhibitor binding kinetics

  2021cites this paper
• Methods for the Construction of Collagen-Based Triple-Helical Peptides Designed as Matrix Metalloproteinase Inhibitors.

  2019cites this paper
• A Primary Evaluation of Potential Small‐Molecule Inhibitors of the Astacin Metalloproteinase Ovastacin, a Novel Drug Target in Female Infertility Treatment

  2019cites this paper
• Matrix Metalloproteinase Triple-Helical Peptide Inhibitors: Potential Cross-Reactivity with Caspase-11

  2019cites this paper
• Second Generation Triple-Helical Peptide Inhibitors of Matrix Metalloproteinases.

  2017cites this paper
• A: An Ideal Target for Anti-virulence Drug Development

  2017cites this paper
• Phosphinic peptides as potent inhibitors of zinc-metalloproteases.

  2016cites this paper
• Matrix Metalloproteinase Inhibition by Heterotrimeric Triple‐Helical Peptide Transition State Analogues

  2015cites this paper
• Identification and activity of inhibitors of the essential nematode-specific metalloprotease DPY-31

  2015cites this paper
• Sortase A: an ideal target for anti-virulence drug development.

  2014cites this paper
• Astacins: proteases in development and tissue differentiation

  2013cites this paper
• Chapter 188 – Astacin

  2013cites this paper
• Biochemical Characterization of a Novel Aspartic Protease from Plutella xylostella, Diamondback moth (Lepidoptera: Plutellidae) Midgut: Inactivation by an Aspartic Protease Inhibitor

  2012cites this paper
• Slow-tight binding inhibition of pepsin by an aspartic protease inhibitor from Streptomyces sp. MBR04.

  2012cites this paper
• A novel bifunctional peptidic aspartic protease inhibitor inhibits chitinase A from Serratia marcescens: Kinetic analysis of inhibition and binding affinity.

  2010cites this paper
• The astacin family of metalloproteinases

  2009cites this paper
• Meprins, membrane-bound and secreted astacin metalloproteinases.

  2008cites this paper
• Synthetic active site-directed inhibitors of metzincins: achievement and perspectives.

  2008cites this paper
• Triple-helical transition state analogues: a new class of selective matrix metalloproteinase inhibitors.

  2007cites this paper
• Biochemical characterization of a low molecular weight aspartic protease inhibitor from thermo-tolerant Bacillus licheniformis: kinetic interactions with Pepsin.

  2006cites this paper
• A conserved tyrosine residue of Saccharomyces cerevisiae leukotriene A4 hydrolase stabilizes the transition state of the peptidase activity.

  2006cites this paper
• Modeling binding kinetics at the Q(A) site in bacterial reaction centers.

  2005cites this paper
• Inhibition of the Staphylococcus aureus sortase transpeptidase SrtA by phosphinic peptidomimetics.

  2004cites this paper
• Inhibition of 1,4-beta-D-xylan xylanohydrolase by the specific aspartic protease inhibitor pepstatin: probing the two-step inhibition mechanism.

  2004cites this paper
• Inhibition of procollagen C-proteinase: fibrosis and beyond

  2004cites this paper
• Fas-disabling small exocyclic peptide mimetics limit apoptosis by an unexpected mechanism.

  2004cites this paper
• Slow Tight Binding Inhibition of Proteinase K by a Proteinaceous Inhibitor

  2003cites this paper
• Phosphorus-based SAHA analogues as histone deacetylase inhibitors.

  2003cites this paper
• Slow-Tight Binding Inhibition of Xylanase by an Aspartic Protease Inhibitor

  2002cites this paper
• Characterization of the proteolytic enzymes in the midgut of the European Cockchafer, Melolontha melolontha (Coleoptera: Scarabaeidae).

  2002cites this paper
• Phosphinic peptide inhibitors of macrophage metalloelastase (MMP-12). Selectivity and mechanism of binding.

  2001cites this paper
• Slow inhibition of almond beta-glucosidase by azasugars: determination of activation energies for slow binding.

  2001cites this paper
• Structural and mechanistic insight into the inhibition of aspartic proteases by a slow-tight binding inhibitor from an extremophilic Bacillus sp.: correlation of the kinetic parameters with the inhibitor induced conformational changes.

  2001cites this paper
• Investigation of the slow inhibition of almond beta-glucosidase and yeast isomaltase by 1-azasugar inhibitors: evidence for the 'direct binding' model.

  2000cites this paper
• Rationally designed anti-HER2/neu peptide mimetic disables P185HER2/neu tyrosine kinases in vitro and in vivo

  2000cites this paper
• Phosphinic acid compounds in biochemistry, biology and medicine.

  2000cites this paper
• Novel methodology for the solid-phase synthesis of phosphinic peptides

  2000cites this paper
• Phosphinic peptide inhibitors as tools in the study of the function of zinc metallopeptidases.

  2000cites this paper
• Proteinase inhibitors and activators: strategic targets for therapeutic intervention

  2000cites this paper
• Phosphinic Peptide Libraries for Proteolytic Enzymes

  1999cites this paper
• RXP 407, a phosphinic peptide, is a potent inhibitor of angiotensin I converting enzyme able to differentiate between its two active sites.

  1999cites this paper
• Kinetic analysis of enzyme reactions with slow-binding inhibition.

  1999cites this paper
• A convenient method to synthesize phosphinic peptides containing an aspartyl or glutamyl aminophosphinic acid. Use of the phenyl group as the carboxyl synthon

  1999cites this paper
• cDNA cloning, bacterial expression, in vitro renaturation and affinity purification of the zinc endopeptidase astacin.

  1999cites this paper